Method of achieving accelerated fat loss by administration of a fat loss accelerating agent to a dieting mammal

ABSTRACT

Accelerating fat loss by administering to a dieting mammal the fat loss accelerating agent 7-oxo DHEA or a pro-drug thereof incapable of in vivo conversion to testosterone.

This application claims the benefit of U.S. Provisional Application No.60/439,816, filed Jan. 13, 2003.

FIELD OF INVENTION

The invention relates to methods of achieving fat loss.

BACKGROUND

The steroid Δ5-androstene-3-ol-7,17-dione (7-oxo DHEA) is believed tostimulate various beneficial biological responses including (i) inducingthe synthesis of various thermogenic enzymes which are effective forregulating metabolism and thereby promoting weight control withoutaffecting caloric intake, and (ii) inducing the synthesis of the majorthyroid hormone triiodothyronine (T₃) which is effective for increasingthe basal metabolic rate and thereby promoting weight control withoutaffecting caloric intake.

The ability of 7-oxo DHEA to promote weight control is widely believedto be mediated through enhanced thermogenesis (conversion of foodstuffsto heat energy rather than chemical energy such as ATP and/ortriacylglycerides). The thermogenic effect mediated by 7-oxo DHEA isbelieved to result from the ability of 7-oxo DHEA to stimulate thesynthesis of thermogenic enzymes including mitochondrial glycerol3-phosphate dehydrogenase (G3P-DH), cytosolic malic enzyme (ME) andfatty acyl CoA oxidase. Such enzymes tend to reduce the efficiency ofenergy metabolism within the body.

While highly effective for safely promoting weight control, a continuingneed exists for achieving accelerated fat loss.

SUMMARY OF THE INVENTION

Fat loss can be accelerated during dieting by the administration of afat loss accelerating agent while dieting. The fat loss acceleratingagent is 7-oxo DHEA or a pro-drug thereof incapable of in vivoconversion to testosterone.

DETAILED DESCRIPTION OF A PREFERRED EMBODIMENT

Definitions

As utilized herein, including the claims, the term “dieting” meanseating and drinking sparingly with the intent to lose weight.

As utilized herein, including the claims, the term “7-oxo DHEA” meansΔ5-androstene-3-ol-7,17-dione.

As utilized herein, including the claims, the term “3-acetyl 7-oxo DHEA”means Δ5-androstene-3-acetoxy-7,17-dione.

Description

I have surprisingly discovered that 7-oxo DHEA is effective foraccelerating the loss of fat during dieting. Without intending to belimited to any particular theory, I believe that the administration of7-oxo DHEA to a dieting mammal is effective for accelerating the loss offat because 7-oxo DHEA modulates the metabolism of the dieting mammal.It is widely believed that dieting is an ineffective means for achievingfat loss because the body reacts to the reduced caloric intake byslowing down the metabolism of the dieter. By modulating the metabolismof the dieting mammal, 7-oxo DHEA would be effective for preventing orat least moderating any diet-induced decrease in the metabolism andthereby accelerate fat loss achievable by dieting.

The Fat Loss Accelerating Agent

The fat loss accelerating agent effective for accelerating the loss offat when combined with dieting is the steroid Δ5-androstene-3β-ol-7,17dione (7-oxo DHEA). 7-oxo DHEA is a derivative of dehydroepiandrosterone(DHEA). 7-oxo DHEA does not appreciably stimulate, increase or otherwiseenhance the production of sex hormones. The steroid is commerciallyavailable from a number of sources including Steraloids, Inc. of Wilton,N.H. A number of procedures are available for synthesizingΔ5-androstene-3β-ol-7,17 dione from DHEA, with one such proceduredescribed in U.S. Pat. No. 5,296,481.

Pro-drugs of 7-oxo DHEA (i.e., compounds readily metabolized in vivo tothe active 7-oxo DHEA) may also be usefully employed. One example of apro-drug is the commercially available Δ5-androstene-3β-acetyl-7,17dione (3-acetyl 7-oxo DHEA). The 3Δ-acetyl group is hydrolyzed in vivoby esterases located in the blood and various tissue to produce theactive 7-oxo DHEA, and is believed to be less susceptible to oxidationduring the manufacturing process relative to 7-oxo DHEA. Other suitablepro-drugs include Δ5-androstene-3β,17β-diol-7-one,Δ5-androstene-3β,7α-diol-17-one, Δ5-androstene-3β,7β-diol-17-one and thecorresponding acetyl esters of these steroids.

Administration

Administration Route

The fat loss accelerating agent can be administered by virtually any ofthe commonly accepted practices for the administration of pharmaceuticalpreparations including specifically, but not exclusively, mucosaladministration, oral consumption, ocular administration, subcutaneousinjection, transdermal administration, etc. Oral administration isgenerally preferred.

Mucosal administration of the fat loss accelerating agent includes suchroutes as buccal, endotracheal, nasal, pharyngeal, rectal, sublingual,vaginal, etc. For administration through thebuccal/sublingual/pharyngeal/endotracheal mucosal, the fat lossaccelerating agent may be formulated as an emulsion, gum, lozenge,spray, tablet or an inclusion complex such as cyclodextrin inclusioncomplexes. Nasal administration is conveniently conducted through theuse of a sniffing powder or nasal spray. For rectal and vaginaladministration the fat loss accelerating agent may be formulated as acream, douche, enema or suppository.

Oral consumption of the fat loss accelerating agent may be effected byincorporating the fat loss accelerating agent into a food or drink, orformulating the fat loss accelerating agent into a chewable orswallowable tablet or capsule.

Ocular administration may be effected by incorporating the fat lossaccelerating agent into a solution or suspension adapted for ocularapplication such as drops or sprays.

Subcutaneous administration involves incorporating the fat lossaccelerating agent into a pharmaceutically acceptable and injectablecarrier.

For transdermal administration, the fat loss accelerating agent may beconveniently incorporated into a lipophilic carrier and formulated as atopical crime or adhesive patch.

Dose Rate

The range of dosages and dose rates effective for achieving the desiredaccelerative fat loss effect may be determined in accordance withstandard industry practices.

1. A method of achieving accelerated fat loss comprising administrationof a fat loss accelerating agent to a dieting mammal wherein the fatloss accelerating agent is 7-oxo DHEA or a pro-drug thereof incapable ofin vivo conversion to testosterone.
 2. The method of claim 1 wherein thefat loss accelerating agent is administered orally.
 3. The method ofclaim 2 wherein the fat loss accelerating agent is administered at leastonce daily.
 4. The method of claim 1 wherein the dieting mammal is ahuman.
 5. The method of claim 2 wherein the dieting mammal is a human.6. The method of claim 3 wherein the dieting mammal is a human.
 7. Themethod of claim 4 wherein the fat loss accelerating agent is 3-acetyl7-oxo DHEA or 3-ester thereof.
 8. The method of claim 5 wherein the fatloss accelerating agent is 3-acetyl 7-oxo DHEA or 3-ester thereof. 9.The method of claim 6 wherein the fat loss accelerating agent is3-acetyl 7-oxo DHEA or 3-ester thereof.